EA201170792A1 - DERIVATIVES OF MORFIN-6-GLUCURONIDE, THEIR RECEIVING AND THEIR APPLICATION IN THERAPY - Google Patents

DERIVATIVES OF MORFIN-6-GLUCURONIDE, THEIR RECEIVING AND THEIR APPLICATION IN THERAPY

Info

Publication number
EA201170792A1
EA201170792A1 EA201170792A EA201170792A EA201170792A1 EA 201170792 A1 EA201170792 A1 EA 201170792A1 EA 201170792 A EA201170792 A EA 201170792A EA 201170792 A EA201170792 A EA 201170792A EA 201170792 A1 EA201170792 A1 EA 201170792A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
therapy
alkyloxy
halo
glucuronide
Prior art date
Application number
EA201170792A
Other languages
Russian (ru)
Other versions
EA019053B1 (en
Inventor
Ален Длюбала
Изабелль Рипош
Клер Трекан
Original Assignee
Санофи
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Санофи filed Critical Санофи
Publication of EA201170792A1 publication Critical patent/EA201170792A1/en
Publication of EA019053B1 publication Critical patent/EA019053B1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/08—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/06—Heterocyclic radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Настоящее изобретение относится к производным морфин-6-глюкуронида следующей формулы (I), в которой R1 обозначает 5-членную гетероароматическую группу, возможно, замещенную одним или несколькими заместителями, выбранными из атомов галогена и (C-C)алкила, галогена, гидроксила, оксо, гало(C-C)алкила, гало(C-C)алкилокси, (C-C)алкилокси, арил(C-C)алкила и арила, причем указанная арильная группа, возможно, замещена одной или несколькими группами, выбранными из групп: (C-C)алкила, гало(C-C)алкила, гидроксила и (C-C)алкилокси, в виде основания или соли присоединения с кислотой, а также в виде гидрата или сольвата. Настоящее изобретение также относится к способу их получения и их применению в терапии.The present invention relates to morphine-6-glucuronide derivatives of the following formula (I), in which R1 is a 5-membered heteroaromatic group, optionally substituted with one or more substituents selected from halogen atoms and (CC) alkyl, halogen, hydroxyl, oxo, halo (CC) alkyl, halo (CC) alkyloxy, (CC) alkyloxy, aryl (CC) alkyl and aryl, wherein said aryl group is optionally substituted with one or more groups selected from the groups: (CC) alkyl, halo (CC ) alkyl, hydroxyl and (CC) alkyloxy, in the form of a base or an addition salt with an acid, and also in the form of hydrate or solvate. The present invention also relates to a method for their preparation and their use in therapy.

EA201170792A 2008-12-10 2009-12-08 Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics EA019053B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0806949A FR2939437B1 (en) 2008-12-10 2008-12-10 MORPHINE-6-GLUCURONIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE
PCT/FR2009/052448 WO2010067010A2 (en) 2008-12-10 2009-12-08 Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics

Publications (2)

Publication Number Publication Date
EA201170792A1 true EA201170792A1 (en) 2012-01-30
EA019053B1 EA019053B1 (en) 2013-12-30

Family

ID=41031604

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170792A EA019053B1 (en) 2008-12-10 2009-12-08 Derivatives of morphine-6-glucuronide, preparation method thereof and use of same in therapeutics

Country Status (30)

Country Link
US (1) US8461122B2 (en)
EP (1) EP2376512B1 (en)
JP (1) JP5616356B2 (en)
KR (1) KR20110104486A (en)
CN (1) CN102317301B (en)
AR (1) AR074514A1 (en)
AU (1) AU2009326909B2 (en)
BR (1) BRPI0922733A2 (en)
CA (1) CA2746429A1 (en)
CL (1) CL2011001399A1 (en)
CR (1) CR20110306A (en)
EA (1) EA019053B1 (en)
EC (1) ECSP11011110A (en)
ES (1) ES2468990T3 (en)
FR (1) FR2939437B1 (en)
HK (1) HK1163110A1 (en)
HN (1) HN2011001601A (en)
IL (1) IL213381A (en)
MA (1) MA32952B1 (en)
MX (1) MX2011006252A (en)
MY (1) MY152978A (en)
NI (1) NI201100115A (en)
NZ (1) NZ593344A (en)
PE (1) PE20120260A1 (en)
SG (1) SG172068A1 (en)
TN (1) TN2011000266A1 (en)
TW (1) TW201026312A (en)
UA (1) UA104302C2 (en)
WO (1) WO2010067010A2 (en)
ZA (1) ZA201104305B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103421063B (en) * 2012-05-23 2016-04-06 宜昌人福药业有限责任公司 A kind of method of synthesizing morphine-6-β-D-Glucose aldehydic acid glycosides
CN111346104B (en) * 2018-12-21 2022-06-10 宜昌人福药业有限责任公司 Morphine-6-glucuronide transdermal drug delivery pharmaceutical composition, preparation method and application thereof

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3766188A (en) 1971-06-28 1973-10-16 Yamanouchi Pharma Co Ltd Carbonyldioxymorphinan derivatives
GB9116909D0 (en) 1991-08-06 1991-09-18 Salford Ultrafine Chem & Res Morphine derivatives
GB2282758A (en) 1993-08-23 1995-04-19 Euro Celtique Sa Oral morphine-6-glucuronide compositions
AU723859B2 (en) * 1997-04-14 2000-09-07 Ufc Limited Morphine derivatives
EP1086114B1 (en) 1998-06-06 2002-10-02 CeNeS Limited Morphine-6-glucuronide synthesis
GB0218811D0 (en) * 2002-08-14 2002-09-18 Cenes Ltd Salts of morphine-6-glucuronide
FR2864082B1 (en) * 2003-12-22 2006-03-10 Synt Em NEW MORPHINE-6-GLUCURONIDE DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME AND USE THEREOF FOR THE TREATMENT OF PAIN
ES2623362T3 (en) * 2004-05-28 2017-07-11 Human Biomolecular Research Institute Metabolically stable pain relievers and pain medications
FR2907121B1 (en) * 2006-10-12 2012-05-04 Neorphys NEW MORPHINIC DERIVATIVES

Also Published As

Publication number Publication date
MX2011006252A (en) 2011-11-04
WO2010067010A2 (en) 2010-06-17
HN2011001601A (en) 2013-09-16
CA2746429A1 (en) 2010-06-17
IL213381A (en) 2014-02-27
JP2012511553A (en) 2012-05-24
FR2939437B1 (en) 2010-12-17
CL2011001399A1 (en) 2011-10-28
WO2010067010A3 (en) 2011-06-30
EP2376512B1 (en) 2014-02-26
CR20110306A (en) 2011-09-21
CN102317301B (en) 2015-08-26
BRPI0922733A2 (en) 2016-01-05
IL213381A0 (en) 2011-07-31
ES2468990T3 (en) 2014-06-17
FR2939437A1 (en) 2010-06-11
AR074514A1 (en) 2011-01-19
CN102317301A (en) 2012-01-11
ZA201104305B (en) 2012-10-31
EA019053B1 (en) 2013-12-30
JP5616356B2 (en) 2014-10-29
MA32952B1 (en) 2012-01-02
ECSP11011110A (en) 2011-07-29
TN2011000266A1 (en) 2012-12-17
AU2009326909A1 (en) 2011-06-30
US8461122B2 (en) 2013-06-11
NZ593344A (en) 2013-08-30
MY152978A (en) 2014-12-15
UA104302C2 (en) 2014-01-27
EP2376512A2 (en) 2011-10-19
KR20110104486A (en) 2011-09-22
NI201100115A (en) 2011-12-14
SG172068A1 (en) 2011-07-28
TW201026312A (en) 2010-07-16
AU2009326909B2 (en) 2016-05-26
HK1163110A1 (en) 2012-09-07
US20110301107A1 (en) 2011-12-08
PE20120260A1 (en) 2012-04-13

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU